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mykw Flashcards

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1
Q

Common mechanisms of Drug resistance?

A

Spontaneous mutations in target proteins, Natural enzymes that inactivate agent, Spontaneous changes in membrane permaability

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2
Q

Molecular Targets for Antimicrobial drugs

A

Cell Wall synthesis, DNA gyrase, DNA-Direction RNA polymerase, Protein synthesis, Cell membrane, Folic acid metabolism, Periplasmic space

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3
Q

Gram negative vs Gram positive

A

Gram negative has small cell wall, gram positive have big cell wall

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4
Q

B-lactam anibiotic classes

A

Cephalosporins and penicillins

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5
Q

Mechanism of Beta-lactam Action

A

Bind to Pencillin binding proteins, Inhibits peptidoglycan synthesis, Stimulates Autolysins, results in cell lysis

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6
Q

Beta Lactams are inactivated by?Static or cidal?Most effective against Gram pos or Neg?

A

B-lactamASES, Gram positive but can have effect on negative

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7
Q

What is the allergen from Pencillins?

A

Penicillinoic acid

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8
Q

Natural Pencillins, Route, and Target, CNS penetration?

A

G, V, G (Benzathine), G is iv/im, V is oral, G B is IM long acting. Gram positive. No CNS

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9
Q

What does MRSA really stand for?

A

Resistant to all Beta lactams

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10
Q

Semisynthetic Pencillins ases resistant, route, used for? CNS penetration?

A

Nafcillin, Dicloxacillin.. Good CNS with meniges inflammation

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11
Q

Semisynthetic Pencillins (Extended spectrum). Route, Spectrum? Combination of?

A

Amoxicillin, Ampicillin, Piperacillin Extended to Gram + and some Gram -. Combination of minopencillin + Beta-lactamase inhibitor(Clavulanate, Sulbactam,Tazobactam)

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12
Q

Synthetic Penicillin-Like (Carbapenems), Spectrum? Co-admined with?

A

Imipenem/Cilastatin. Broadest spectrum Most + and - . Coadministered with Cilastatin. Inhibitor of the degradation renal enzymes

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13
Q

Semi-synthetic monobactams. Spectrum? Not affected by?What patients?

A

Aztreonam. Inhibits PBP of Gram NEGATIVE ONLY, beta lactamases. Good for B-lactam allergic patients with gram negative

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14
Q

Cephalosporins are used as what in hospital settings?Natural product of?

A

Prophylaxis, molds

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15
Q

1st Generation Cephalorsporins, Specrum, Used for?

A

Cephazolin (Ancef), Cephalexin (Keflex), Gram + and Some gram -, Surgical prophylaxis, UTI

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16
Q

2nd Generation Cephalorsporins, Spectrum? Used for?

A

Cerfuroxime (Zinacef), Cefuroxime axitel (Ceftin), Intermediate Spectrum. Gram + and extended Gram Negative.

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17
Q

Third Generation Cephalorsporins. Spectrum? Used for? Special consideration?

A

Ceftriaxone (Rocephin), Ceftazidime (Fortaz), Broad spectrum Gram + and Gram Negative. CNS penetration

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18
Q

Fourth Generation cephalosporins. Spectrum? Used for?

A

Cefepime (Maxiprime). Very broad Gram + and Negative. Aerobic. Used for limited resistants and nosocomial infections

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19
Q

B-Lactam adverse reactions. 3 stages and effects

A

1st immediate= anaphylaxis <72 hours Milder, maybe rash. 3rd is Late reaction Drug fever

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20
Q

Tetracycline bacteriostatic or bacteriocidal?

A

Static

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21
Q

Tetracycline mechanism

A

Blocks tRNA bind=Block protein synthesis 30s

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22
Q

Tetracycle spectrum? UV? Divalent metals?

A

Very broad spectrum. Forms complexes with Teeth and Bones. Absorbs UV causing inflammatory response

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23
Q

Chloramphenicol block wwhat ribsome?

A

50s

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24
Q

Chloramphenicol spectrum? Cidal or static? Alternative for?

A

Extremely broad. Static. Alternative to Beta lactams for CNS

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25
Chloramphenicol side effects bone marrow? Babys?
Grey baby, Bone marrow toxicity
26
Macrolide/Ketolides block what ribsome?Static or cidal?Spectrum?
50S, static, NO CNS, Gram positive with limited negative
27
Macrolide and Ketolide Protoypes
Erythromycin, Azithromycin, Clarithrymycin, Telithromycin, Clindamycin
28
Polumyxin spectrum? Acts on? Static or cidal? ROUTE?
Gram Negative bacteria. Acts on lipid membrane. BacteriCIDAL, TOPICAL only
29
Bacitracin Route? Spectrum? Mechanism?
Topical only. Limited to Gram positive. Blacks cell wall synthesis
30
Vancomycin Route? Spectrum? Mechanism?
IV/IM, Limited to Gram positive. Blocks cell wall synthesis
31
Inhibitors of Cell wall synthesis?
Bactracin and vancomycin
32
Tigecycline is for? Spectrum? Mechamism?Class?
Resistant strains. Tetracyline. Blocks tRNA binding on 30s ribosome. Broad + and - spectrum
33
Quinupristin/Dalfopristin (Synercid). Spectrum? Class? Used for? Mechanism?
Blocks protein synthesis on 30s ribosome. Used for ONLY Gram positive. For resistant Vanomycin strains. Macrolide class
34
Linezolid. Spectrum?Class? Used for? Mechanism?
Oxazolidone class. Blocks protein synthesis at TRNA formation. Broad against Gram positive. For VRSA
35
Daptomycin. Class?Spectrum?Used for?
Natural derived class. Used for MRSA and VRE. Gram positive
36
Mercaptopurine mechanism, converted to?
Blocks purine synthesis by being an analog of purine bases hypoxanthine or adenine, T-IMP
37
Azathioprine is?
prodrug of 6-MP
38
Methotrexate mechanism, inhibits what enzyme and synthesis
Inhibits dihydrofolate redutase and inhibits synthesis of thymidine and purines
39
5-Flurouracil mechanism, inhibits what? Inhibits synthesis of what?
Inhibits thymidylate synthase, inhibiting synthesis of thymidine
40
Hydroxyurea inhibits what?
ribonucleotide reductase
41
Anti-microtubules are considered to be what phase specific agents?
M phase
42
Anti dna nucleotide synthesis is for what phase?
G1
43
Vinca alkaloids mechanism? Vincristine, Vinblastine, Vinorelbine
Binds to tubulin and inhibit tublin polymerization
44
Taxanes (Paclitaxel, Docetaxel) mechanism
prevent depolymerization
45
Anthracyclines (doxorubicin, Daunorubicin mechanism
Insert into DNA, inhibits topoisomerase II and induce production of ROS. Deforming DNA
46
Bleomycin (blenozane, Cipla, Bleocip), anesthesia concerns
Requires metal and oxygen for its activity, causes DNA damage by producing ROS. Causes pulmonary fibrosis
47
Nitroden mustards:cyclophosphamide
Alklyating agents, crosslinking DNA.
48
Tamoxifen is?
Selective estrogen receptor modulator for breast cancer
49
Aromtase inhibitor (Anastrozole)
Blocks estrogen synthesis
50
Imatinib (Gleevec)
Inhibits Tyrosine kinase inhibitor for Chronic myeloid leukemia
51
Trastuzumab (Herceptin)
Monoclonal antibody against HER2, for breast cancer, cardiotoxic
52
Bevacizumab (Avastin)
Monoclomal antibody againsst Angiogensis
53
FDA Pregnacy rating ABCDX
A, adequate studies show no risk, B Animal studies fail to show risk, no study in human. C-Animals positive, no studies Human. D-Positive in human studies but may be used. X-Animals/Human positive and risks outweight benefits. N-No classification
54
Thalidomide concerns, which enantomer?
Presciped for pregnacy associated nausea, bilateral limb reduction, kidney eyes ears heart deformities. S enantiomer
55
Diethylstilbesterol (DES)
Oral synthetic nonsteroidal estrogen analog, Use to prevent miscarriages. Teratogen seen 20-30 years later
56
Fetal Alcohol syndrome
Most common cause of mental retardation, completely preventable
57
Phenytoin (Dilatin)
Antiepileptic medicationm, will show and resemble FAS (feal alcohol syndrome), epoxide hydrolase 1. Fetal Hydantoin syndrome
58
Mechanism of Nicotine/Tobacco tetragenic effects
Growth retardation, restrictions uterine blood vessels chronic hypoxia and malnutrition
59
Retinoids Isotretinoin(acutane)
Vitamin A analog, for acne causing fetal abnormality
60
Gamma Globulin (IgG) mechanism viruses
Blocks the attachment of virus particles to host cells
61
Amantadine rimantadine
Targets m2 protein of influeza A virus and prevents uncoating of vesicle by blocking acidification of vesicle
62
Oseltamivir (Tamiflu
Targets influenza A and B and prevents replication and host cleavage from host cell nueraminidase inhibitor. Inhibits respiratory spread
63
Acyclovir mechanism, what is needed for it to work? Prodrug?
Inhibits viral dna polymerase, requires viral hymidine kinase for activation. Used for herpes infections
64
Forscarnet mechanism and uses
Effective against herpes simplex virus that are deficient in thymidine kinase, used for cytomegalovirus reitinitis and acyclovir ressitant herpes
65
Ribavirin uses
Used for chronic treatment of hep C and respiratory syncytial virus
66
Zidovudine (AZT)
Emtricitabine-reverse transcriptase inhibitors
67
Fuzeon mechanism
Interferes with Entry of HIV-1 into cells. Inhibits fusion or viral and cellular membranes
68
Amophotericin B spectrum and mech, side effect
broad spectrum severe antifungal agent, big ring structure and one side is hydrophobic because it binds to membrane creating a channel to lose intracellular components. Renal toxicity
69
Griseofukvin mechanismm spectrum?
Binds to microtubules causing nterference with mitotic spingle formation and dividing cells, narrow spectrum, atheletes foot
70
Azole mechanism
Inhibits ergosterol synthesis, leading to damaged and leaking cell membranes
71
Fluconazole mechanism, spectrum class
Very broad spectrum for most candida. single oral fose for yeast infection. For fungal meningiutis, high concentration in CNS. Triazoles
72
Voriconazole for what?
active against molds such as aspergillus, for invasive aspergillosis
73
Itraconazole spectrum, interesting properities?
broad spectrum, low gastric pH for absorption
74
Posaconazole uses
prevent candida and aspergillus infections in immunocompromised patients
75
Ketoconazole what class? For?
Class imidazole, broad spectrum effective against fungi
76
Amtimetabolite drug, uses in combination with
for systemic fungal infection such as cryptococcal menigitis, combination with amphotericin B
77
New class of antifungal agents
Glucan synthase inhibitors, the echinocandins
78
Enchinocandins, Glucan synthase inhibitors
Caspofungin, blocks cell wall synthesis, micafungin, anidulafungin
79
Schedule I drugs
High potential for abuse and no approved medical use such as heroin
80
Schedule II drugs
high potential for abuse but has accepted medical use such as morphine, oxycodone. No automatic refills
81
Scheduled III drugs
Moderate potential for abuse and refills can happen 5 times in 6 months
82
Schedule 4 drugs
lower potential for abuse and same regulations as 3
83
Schedule V drugs
limited potential for abuse, no dispense and refils
84
IND application is?
Investigational New drug. Preclinical data, trial design, informed consent form
85
Phase 0 clinical trials
microdosing trials, sub therapeutic dose and kinetic and dynamic data
86
Phase 1 clinical trials
Tests safety of drug not efficiacy.
87
Phase 2 trials
Tests for safety and efficacy,
88
Phase 3
Randomized efficacy is compared to the standard treatment
89
NDA is?
establishment of DA sets standards for the safety of the ingredients of the drug, labeling and package insert
90
Phase 4 clinical trial
additional safety data, or additional uses or in combination with other drugs, increase the "label" of the drug
91
5 Diuretic classes
Carbonic anhydrase inhibitor, thiazides, osmotics, K sparing, loops
92
2 high ceiling dieurtics
Loop and osmotics
93
3 low ceiling dieurtics
K sparing, carbonic anhydrase inhibitor, thiazides
94
Carbonic anhydrase inhibitor site of action and mechanism. Prototype
Increased bicarb rentention in the proximal tubule, Acetazolamide
95
Osmotic dieuretic protoype and location and mechanism
Proximal tubule and descending loops of henle, Mannitol, increases water excretion
96
Loop dieurtic protoype, site of action, mechianism
Furosemide (Lasix), loop of henle. Blocks na k and cl reabsorption
97
Thiazides site of action, mechanism, protoype, side effect
Distal tubule, blocks Na cl co transporter.hypokalemia. Hydrochlorothiazide
98
K+ sparing dieurtics, mechanism, site and prototype
Collecting duct, blocks Na+ channel, can cause hyperkalemia. Triamteren and amiloride
99
K+ sparing dieurtic that Is an antagonist of aldosterone receptor
Spironolactone
100
How do dieurtics cause hypokalemia?
Increased NA reabsorption causes excess K excretion
101
Aminoglycosides cidal or static? Mechanism?
Cidal, block protein synthesis
102
Aminoglycosides used for?
Aerobic gram negative bacteria
103
Streptomycin history and primary use
Multidrug resistant TB, first amingolycoside to be developed
104
Isoniazid use, mechanism
mycolic acid synthesis inhibition, for TB
105
Rifampin mechanism and uses, side effects
TB gram +- and inhibits RNA synthesis and inhibits RNA polymerase in prokaryotic cells, liver toxicity
106
Ethambutol used for only? Static or cidal, indications for use
Only for mycobacteria, bacteriostatic, has to be used in combination
107
Pyrazinamide uses, mechanism and interesting factor
active at acidic ph, used for TB, inhibits fatty acid synthesis
108
Is combination therapy mandatory for TB?
Yes
109
Lunelle dosage and frequency
Estradiol and medroxyprogesterone injection every ~30 days
110
Nuvaring contents
Ethinyl estradiol
111
Orthoevra contents, rsk
E+ P, worn for 7 days, patch risk of blood clots
112
Ctinuous E + p pill, no period
Lybrel
113
Yasmin contents and side effects
drospirenone plus ethinlestradiol, hyperkalemia, heart problems DVT
114
Progrestin alone therapy does what
Endometrial changes, thickening of mucus, prevents ovulation
115
Progesterin only drugs
Minipill, depo provera, mirena, implanon
116
Clomiphere uses and mechianism
fertility pill, estrogen receptor antagonist
117
Tamoxifen class, what for
SERM, breast cancer
118
Raloxifene for? Does what
Estrogen antagonist in breast and uterin, agonist in bone. Prevents osteroporosis post menopausal
119
Femara use, mechanism
Aromatase inhibitor, reduces estrogen production for breast cancer treatment
120
4 synthetic corticosteroids
prednisone, prednisolone, dexamethasone, betamethasone
121
Echanism of action of corticosteroids
gene regulation
122
Is alderstrone part of the pituary axis?
no, renin angiotensin
123
Treatment of adrenocortical insuffieciency
cortisol
124
Treatment of inflammation and immunosuppression
Intermediate and long acting
125
Mineralcorticoids effects
salt rention and hypertension
126
Most widely used mineralcorticoid
fludrocortisone
127
Inhibition of adrenal cortical steroids
aminoglutethimide
128
Treatment of hypothroidism
Levothryoxine or Liothyronine, Synthroid or L-t3
129
Graves is?
caused by hyperthroidism
130
Drug of choice for thryoid storm
propanolol
131
Sulfonamides inhibti what? Clinical use?
synthesis of dihydropteroate, burn patients, inflammatory disorder of GIT, respiratory infection UTI
132
Trimethoprime mechanism, incombination with
inhibits reductase enzyme for tetrahydrofolate, co0trimoxazole
133
Fluoroquinolones mechanism, spectrum?
inhibit DNA gyrase, Gram negative aerobic
134
Fluoroquinolones drugs
Ciprofoxacin (anthrax),
135
How does mylanta work?
decrease acid in stomach
136
Mucosal protectants from acid in stomach
Peptobismol, Misoprostol, Sucralfate
137
H2 receptor antagonist
Cimetidine, Rantitide, Famotidine, Nizatidine
138
Proton pump inhibitors, pro drugs?7
Omeprazole (Prilosec, Lansoprazole Rabeprazole, esomeprazole, all pro drugs
139
Eradication of h.pylori always requires?
multidrug therapy such as PPI, antibiotic 1 and 2, amoxicillin clarithromycin and omeprazol

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